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Literature summary for 5.3.99.3 extracted from

  • Bahia, M.S.; Katare, Y.K.; Silakari, O.; Vyas, B.; Silakari, P.
    Inhibitors of microsomal prostaglandin E2 synthase-1 enzyme as emerging anti-inflammatory candidates (2014), Med. Res. Rev., 34, 825-855 .
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
glutathione
-
Homo sapiens

Application

Application Comment Organism
medicine enzyme inhibition can be useful for treating pain, fever, and anorexia Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in A-549 cells, HeLa cells, HEK-293 cells, RAW 264.7 cells, Pichia pastoris strain KM71H, and Sf9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
-
Homo sapiens
4-(3-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole-5-carboxylic acid
-
Homo sapiens
AF3442
-
Homo sapiens
licofelone
-
Homo sapiens
Oxacillin
-
Homo sapiens
YS121 reversible and noncompetitive inhibition Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Prostaglandin H2 Homo sapiens
-
Prostaglandin E2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
epididymis
-
Homo sapiens
-
epithelial cell
-
Homo sapiens
-
seminal vesicle
-
Homo sapiens
-
Sertoli cell
-
Homo sapiens
-
spermatocyte
-
Homo sapiens
-
spermatogonium
-
Homo sapiens
-
vas deferens ampulla Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Prostaglandin H2
-
Homo sapiens Prostaglandin E2
-
?

Subunits

Subunits Comment Organism
homotrimer
-
Homo sapiens

Synonyms

Synonyms Comment Organism
microsomal prostaglandin E2 synthase-1
-
Homo sapiens
mPGES-1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0034
-
pH and temperature not specified in the publication Homo sapiens YS121
0.006
-
pH and temperature not specified in the publication Homo sapiens licofelone

Expression

Organism Comment Expression
Homo sapiens the enzyme shows elevated levels in the cartilages and chondrocytes of patients suffering from osteoarthritis. The enzyme is overexpressed in 80% of several cancer cells up